AMG-511 is a potent and selective pan class I PI3K inhibitor exhibiting IC50 of 8, 11, 2, and 6 nM against the PI3K β, α, β, and ≤ isoforms respectively. AMG 511 inhibited PI3K pathway signaling in U87 MG glioblastoma cells as determined by dose-dependent reduction in AKT S473 phosphorylation (IC50 = 4 nM). AKT inhibition resulted in a concomitant reduction in PRAS40 phosphorylation (IC50 = 23 nM), a downstream effector of AKT. Reduced phosphorylation of mTORC1 substrates p70S6K (IC50 = 30 nM) and S6 (IC50 = 70 nM) but not 4EBP1 (T37/46), was also detected in U87 MG cells. References: Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J, McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH. Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5630-4. doi: 10.1016/j.bmcl.2014.10.085. PubMed PMID: 25466188.

纯度：≥98%

CAS：1253573-53-3